CONCO

Work Package Leader: Paul CORDOPATIS (University of Patras)

Participants: CEA, University of Patras, Axxam, University of Leuven, University of Utrecht

Lead Optimisation and Structure-Activity Studies

Selected hits generated will be synthesised for in-depth investigations which will include repeated bioassays on a wide range of tests to validate selectivity and potency. Early toxicity in cell-based assays and animal models will be determined, and preliminary in vitro stability assays will be undertaken.

Structure-activity studies will be conducted in parallel with computer-assisted drug design and synthetic analogues will be produced in view to modulate the activity, stability, toxicity and specificity. The most promising hits will then be selected as lead compounds and synthesised with stable isotope labelling for refined high-resolution structural studies by NMR spectroscopy.

This workpackage will be under the supervision of Prof Paul Cordopatis who has a solid expertise in these multidisciplinary fields.